产品描述:
Bufexamac is an NSAID and inhibitor of the class IIb histone deacetylases HDAC6 and HDAC10.{43497} It inhibits the production of IFN-α in peripheral blood mononuclear cells (PBMCs; EC50 = 8.9 µM). Bufexamac induces hyperacetylation of tubulin (IC50 = 2.9 µM), a major substrate of HDAC6, without increasing acetylation of the class I HDAC substrates H3K5 or H3K9/K14. It also inhibits leukotriene A4 (LTA4) hydrolase and aminopeptidase activity (IC50s = 15.86 and 11.59 µM, respectively) and 5-lipoxygenase (5-LO) activity (IC50 = 27 µM).{43498,43499} Bufexamac inhibits the production of leukotriene B4 (LTB4; Item No. 20110) in neutrophils (IC50 = 12.91 µM) and reduces fMLP-induced neutrophil migration when used at concentrations of 50 and 100 µM.{43498} It also reduces neutrophil levels, as well as protein levels of TNF-α and IL-1β, in bronchoalveolar lavage fluid (BALF) in a mouse model of LPS-induced acute lung injury when administered at a dose of 100 mg/kg.